Development of 6-Thioguanine conjugated PLGA nanoparticles through thioester bond formation: Benefits of electrospray mediated drug encapsulation and sustained release in cancer therapeutic applications

Advances in Thiopurine Drug Delivery: The Current State-of-the-Art

“…These approaches include liposomal delivery, micelles, microspheres and metallic and polymeric based nanoparticles (see Fig. 2) [66][67][68][69][70][71][72][73][74][75][76][77].…”

“…Other conjugated polymeric approaches have been described. These include thioguanine-dialdehyde sodium alginate nanoparticles [71], thioguanine-poly-lactic-coglycolic acid (PLGA) nanoparticles [73], azathioprinegelatin nanoparticles [94] and glutathione-sensitive hyaluronic acid-mercaptopurine nanoparticles [69]. Govindappa et al [70] studied the toxicity of mercaptopurine-conjugated chitosan nanoparticles in an animal model.…”

“…These data suggested that mercaptopurine nanoparticles had a favorable toxicity profile compared to normal mercaptopurine drug formulations. Chatterjee et al [ 73 ] investigated thioguanine conjugated PLGA nanoparticles. They obtained an encapsulation rate of 97% and a sustained drug release rate of 60–65% in the first 30 days.…”

Electrospray-based synthesis of fluorescent poly(d,l-lactide-co-glycolide) nanoparticles for the efficient delivery of an anticancer drug and self-monitoring its effect in drug-resistant breast cancer cells

“…The PLGA-PBA polymer was used to fabricate the fluorescent PLGA-PBA nanoparticles by following our previously reported electrospray method. 25 Briefly, the PLGA-PBA polymer was dissolved in acetone (3.0 %, W/V) then stirred for 10 min to form a homogeneous solution. Following the previously reported electrospray method, the polymer solution was dribbled at a flow rate of 0.35 ml/h from a syringe pump through a conductive needle connected with a high voltage power supply.…”

“…In this process, as soon as the electric field intensity reached to the Rayleigh limit, a Taylor cone is formed which undergo Coulomb fission leading to the formation of stable PLGA-PBA nanoparticles. 25 The third or last step deals with the EDA-assisted functionalization of PLGA-PBA nanoparticles with MTX molecule using aminolysis chemistry as reported in our previous publication (Fig. 1).…”